General description
A cell-permeable binaphthol-sulfonamide that competes against pY proteins for Stat3 SH2 domain binding. Shown to inhibit G-CSF-induced (100 ng/ml for 15 min following 1 h drug pretreatment) Stat3 tyr705 phosphorylation in 6 human AML cell lines (IC50 from 4.1 to 8.3 µM) and 4 primary pediatric AML cultures (IC50 from 8 to 18 µM). Long-term treatments (24 h for lines and 48 h for primary cultures) result in apoptosis induction (Annexin V-PE staining) in 7 AML lines (EC50 from 8.4 to 43.6 µM) and CD34+ populations from 5 primary pediatric AML samples (EC50 from 0.8 to25 µM). Selectivity studies using Kasumi-1 cells reveals concomitant inhibitions of G-CSF-stimulated TIE2, MATK, JAK1, and HGFR phosphorylation (by 90%, 50%, 40%, and 40%, respectively; 10 µM C188-9), but not 15 other phosphoproteins (≤30% inhibition), including pERK1/2 and pAKT.
A cell-permeable binaphthol-sulfonamide that competes against pY proteins for Stat3 SH2 domain binding. Shown to inhibit G-CSF-induced Stat3 tyr705 phosphorylation in human AML cell lines and primary cultures (IC50 from 4.1 to 18 µM). Also shown to inhibit G-CSF-stimulated TIE2, MATK, JAK1, and HGFR phosphorylation (by 90%, 50%, 40%, and 40%, respectively; 10 µM C188-9), but not 15 other phosphoproteins (≤30% inhibition), including pERK1/2 and pAKT, in Kasumi-1 cells.
Packaging
Packaged under inert gas
Warning
Toxicity: Toxic (F)
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Redell, M.S., et al. 2011. Blood112, 355.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 471.52. Empirical Formula: C27H21NO5S. Quality Level: 100. Assay: ≥. 98% (HPLC). form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white to pale beige. solubility: DMSO: 100 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: OC1: C(C2: C(O)C: CC3: C2C: CC: C3)C: C(NS(C(C: C4): CC: C4OC)(: O): O)C5: C1C: CC: C5. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 573128-10MG